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Active ingredient: Hydrocodone - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Analgesics
  • Antitussives
  • Narcotics

Dosage Forms

  • Tablets
  • Syrup
  • Liquid mixtures with other analgesics

Brands / Synonyms

Antitussive Hydrocodone and Homatropine Methylbromide; Bekadid; Codinovo; Dico; Dicodid; Dihydrocodeinone; Hidrocodona [Inn-Spanish]; Hycodan; Hycomine; Hycotuss; Hydrocodon; Hydrocodone and Acetaminophen; Hydrocodonum [Inn-Latin]; Hydrocone; Hydroconum; Hydromet; Idrocodone [Dcit]; Lortab; Lortab Elixir; Multacodin ; Tussicaps Extended-Release; Tussigon; Tussionex; Tussionex Pennkinetic Extended-Release; Vicodin; Vicodin ES; Vicodin HP; Vicoprofen; Zydone

Indications

For relief of moderate to moderately severe pain.

Pharmacology

Hydrocodone, a semisynthetic opiate agonist and hydrogenated ketone derivative, is similar to other phenanthrene derivatives, such as codeine. Used as an analgesic, hydrocodone is combined with acetaminophen, ibuprofen, or aspirin to treat pain. Used as an antitussive, hydrocodone is combined with phenylephrine, pseudoephedrine, phenylpropanolamine, guaifenesin, pyrilamine, pheniramine, or chlorpheniramine.

Mechanism of Action

Hydrocodone acts as a weak agonist at OP1, OP2, and OP3 opiate receptors within the central nervous system (CNS). Hydrocodone primarily affects OP3 receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as hydrocodone also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability.

Absorption

Well absorbed from the gastrointestinal tract.

Toxicity

Symptoms of overdose include respiratory depression (a decrease in respiratory rate and/or tidal volume, Cheyne-Stokes respiration, cyanosis), extreme somnolence progressing to stupor or coma, skeletal muscle flaccidity, dizziness, ringing in the ears, confusion, blurred vision, eye problems, cold and clammy skin, and sometimes bradycardia and hypotension. In severe overdose, apnea, circulatory collapse, cardiac arrest and death may occur. LD50=85.7mg/kg (subcutaneous, in mice).

Biotrnasformation / Drug Metabolism

Hepatic and also in intestinal mucosa.

Contraindications

This product should not be administered to patients who have previously exhibited hypersensitivity to hydrocodone or acetaminophen.

Patients known to be hypersensitive to other opioids may exhibit cross-sensitivity to hydrocodone.

Drug Interactions

Patients receiving other narcotic analgesics, antipsychotics, antianxiety agents, or other CNS depressants (including alcohol) concomitantly with hydrocodone and acetaminophen tablets may exhibit an additive CNS depression. When combined therapy is contemplated, the dose of one or both agents should be reduced.

The use of MAO inhibitors or tricyclic antidepressants with hydrocodone preparations may increase the effect of either the antidepressant or hydrocodone.

The concurrent use of anticholinergics with hydrocodone may produce paralytic ileus.

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